Detection of the selective androgen receptor modulator GSK2881078 and metabolites in urine and hair after single oral administration

Detection of the selective androgen receptor modulator GSK2881078 and metabolites in urine and hair after single oral administration / Alina Rading, Patricia Anielski, Detlef Thieme, Annekathrin Martina Keiler. - (Drug Testing and Analysis 13 (2021) 1 (January); p. 217-222)

  • PMID: 33037775
  • DOI: 10.1002/dta.2943


Abstract

Hair and urine concentrations of the nonsteroidal selective androgen receptor modulator GSK2881078 were examined following single oral administration to investigate its hair incorporation and estimate the general suitability of hair testing for selected androgen receptor modulators. Hair segments were collected following a single dose of 1.5 mg GSK2881078 by repeated shaving of scalp hair at Week 0 (blank), Week 1 (representing the pre-application period), Week 3 (ideally focusing the time of incorporation), and Weeks 5 and 9 (post-administration period). The intact compound and various (at least 4) hydroxy-metabolites exhibited similar elimination profiles. The peak urinary concentration (approximately 920 pg/ml) was observed after 8 h and is reduced to the detection limit (2 pg/ml) on Day 42 following administration of 760 μg GSK2881078. Correspondingly, hair concentrations of GSK2881078 (intact compound only) following a single oral dose of 1.5 mg GSK2881078 reached a peak concentration of 1.7 pg/mg in the segments collected 3 weeks post administration, representing the time of ingestion. The concentration rapidly declined to trace amounts of 0.7 (Week 5) and 0.2 pg/mg (Week 9), respectively. In conclusion, measurement of the intact compound GSK2881078 is feasible for both urine and hair analysis. However, concentrations in hair after single oral administration are in the low pg/mg range and can only be detected, if the segments cover the administration period.

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Science
Study
Date
10 October 2020
People
Anielski, Patricia
Keiler, Annekathrin Martina
Rading, Alina
Thieme, Detlef
Country
Germany
Language
English
Other organisations
Technische Universität Dresden (TU Dresden) - Technical University of Dresden
Laboratories
Kreischa, Germany: Institute of Doping Analysis and Sports Biochemistry (IDAS)-Dresden
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Hairtest
Testing method development
Doping classes
S1. Anabolic Agents
Substances
Selective androgen receptor modulators (SARMs)
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Scientific article
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Date generated
22 February 2021
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3 March 2021
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